Correlation between the activities for formation of M2, M4, and M7 and the predetermined activities of P450 enzymes in a panel of individual HLM samples
Individual human liver microsomes were incubated at 5 μM apixaban in the presence of NADPH at 37°C for 60 min. The Pearson correlation coefficients (r) of the predetermined CYP3A4/5 activities with the predetermined 2C8 and 2B6 activities were 0.66 and 0.59, respectively.
Enzyme | Correlation Coefficients (r) | ||
---|---|---|---|
M2 Formation | M4 Formation | M7 Formation | |
CYP1A2 | 0.14 | 0.14 | 0.01 |
CYP2A6 | 0.24 | 0.34 | 0.38 |
CYP2B6 | 0.36 | 0.46 | 0.50* |
CYP2C8 | 0.65* | 0.42 | 0.61* |
CYP2C9 | 0.51* | 0.31 | 0.36 |
CYP2C19 | 0.25 | 0.43 | 0.36 |
CYP2D6 | 0.12 | 0.26 | 0.39 |
CYP2E1 | 0.36 | 0.03 | 0.19 |
CYP3A4/5 | 0.76** | 0.90** | 0.96** |
CYP4A11 | 0.26 | 0.07 | 0.03 |